267641-97-4Relevant academic research and scientific papers
Pyrazole analogues of prazosin
Ermondi, Giuseppe,Boschi, Donatella,Di Stilo, Antonella,Tironi, Carla,Gasco, Alberto
, p. 519 - 524 (1998)
A series of analogues of prazosin, in which 1-methyl or 1- phenylpyrazole moieties were substituted for the furan ring, were synthesized and studied for their α1-adrenoceptor antagonist activity. The role of the five member heterocyclic substru
Anti-inflammatory effect of a new piperazine derivative: (4-methylpiperazin-1-yl)(1-phenyl-1H-pyrazol-4-yl)methanone
Batista, Daniel C.,Silva, Daiany P. B.,Florentino, Iziara F.,Cardoso, Carina S.,Gon?alves, Merita P.,Valadares, Marize C.,Li?o, Luciano M.,Sanz, Germán,Vaz, Boniek G.,Costa, Elson A.,Menegatti, Ricardo
, p. 217 - 226 (2017/10/06)
Aims: This study investigates the anti-nociceptive and anti-inflammatory effects of new piperazine compound (LQFM182) as well as the toxicity acute in vitro. Main methods: To evaluate the anti-nociceptive activity, the acetic acid-induced abdominal writhing test, tail flick test and formalin-induced pain test were used. The anti-inflammatory activity was evaluated using the models of paw oedema and pleurisy induced by carrageenan and some inflammatory parameters were evaluated, including cell migration, myeloperoxidase enzyme activity and the levels of TNF-α and IL-1β cytokines in pleural exudate. The acute oral systemic toxicity of LQFM182 in mice was evaluated through the neutral red uptake (nru) assay. Key findings: LQFM182 (50, 100 or 200?mg/kg, p.o.) decreased the number of writhings induced by acetic acid in a dose-dependent manner, and an intermediate dose (100?mg/kg, p.o.) reduced the paw licking time of animals in the second phase of the formalin test. Furthermore, LQFM182 (100?mg/kg, p.o.) reduced oedema formation at all hours of the paw oedema induced by carrageenan test and in pleurisy test reduced cell migration from the reduction of polymorphonuclear cells, myeloperoxidase enzyme activity and the levels of pro-inflammatory cytokines IL-1β and TNF-α. Therefore, it was classified in GHS category 300?50??2000?mg/kg. Significance: Reduction of the TNF-α and IL-1β levels.
A novel series of potent and selective small molecule inhibitors of the complement component C1s
Subasinghe, Nalin L.,Ali, Farah,Illig, Carl R.,Rudolph, M. Jonathan,Klein, Scott,Khalil, Ehab,Soll, Richard M.,Bone, Roger F.,Spurlino, John C.,DesJarlais, Renee L.,Crysler, Carl S.,Cummings, Maxwell D.,Morris Jr., Philip E.,Kilpatrick, John M.,Babu, Y. Sudhakara
, p. 3043 - 3047 (2007/10/03)
Activation of the classical pathway of complement has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury and acute transplant rejection. The trypsin-like serine protease C1s represents a pivotal upstream point of
The Direct Carboxylation of Pyrazoles
Chiriac, C. I.
, p. 753 - 755 (2007/10/02)
Various pyrazole-4-carboxylic acids 4 were obtained by a direct carboxylation reaction of pyrazoles 1 with excess, oxalyl chloride.
